User:Bilalabualrub/sandbox

 Agonist-antagonist draft 

Background

An agonist is a compound that increases the effect of a neurotransmitter. An antagonist is a compound that decreases the effect of a neurotransmitter. These actions can be achieved via multiple mechanisms. A common mechanism for agonists is re-uptake inhibition, meaning that the agonist blocks neurotransmitters from reentering the pre-synaptic cell. This gives the neurotransmitter more time in the synaptic cleft to act on the synaptic receptors. Antagonists, on the other hand, usually bind directly to receptors in the synaptic cleft, effectively blocking neurotransmitters from binding.

Examples

Buprenorphine is an example of an agonist-antagonist. It is a partial agonist meaning, it activates opioid receptors, but to a much lesser degree than a full agonist, like morphine or fentanyl. It acts as an antagonist by blocking other opioids from binding, while still partially activating the mu opioid receptor. [1]

Sources


 * 1) Kumar, Rachna. “Buprenorphine.” StatPearls [Internet]., U.S. National Library of Medicine, 12 Feb. 2019, https://www.ncbi.nlm.nih.gov/books/NBK459126/.

Corrections

-change sigma to sigma 1 throughout